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,
, Mise au point de nouvelles techniques de radio-iodation et application au radiomarquage de molécules d'intérêt
, En médecine nucléaire, des radiopharmaceutiques pour la thérapie par radio-isotopes (RIT) et des radiotraceurs pour des expériences d'imagerie telles que la TEP (tomographie par émission de positons), la tomographie par émission monophotonique (TEMP) ou la scintigraphie ont été décrites. Plusieurs isotopes de l'iode peuvent être utilisés à la fois pour le diagnostic et le traitement : 123 I pour l'imagerie TEMP, 124 I pour la TEP, 125 I pour l'analyse biologique et 131 I pour la radiothérapie et la scintigraphie. Les méthodes classiques de radio-iodation reposent sur l'utilisation d'un précurseur pré-fonctionnalisé, qui doit être synthétisé, isolé et purifié avant d'être introduit à l'étape de radio-iodation. La méthode par radioiododéstannylation est la méthode la plus populaire, bien que les précurseurs stannylés soient connus pour leur synthèse difficile et leur toxicité. Le développement de nouvelles méthodes de radioiodation représente donc un grand intérêt dans le domaine de la radiochimie, Le radiomarquage de molécules d'intérêt avec des isotopes radioactifs est d'un grand intérêt pour la communauté scientifique, car il influe fortement sur le processus de découverte dans les sciences de la vie et en médecine nucléaire. Les molécules radiomarquées ont été largement utilisées pour évaluer les réactions biochimiques
, Sur la base de la littérature, notre groupe développe actuellement une nouvelle méthode de radioiodation de dérivés d'arylsilanes par radioiododésilylation dans des conditions douces. Cette méthodologie générale permet pour le moment le radiomarquage de dérivés d, Cette stratégie originale permet le radiomarquage de molécules d'intérêt dans des conditions très douces sans utiliser de précurseurs chimiques
, In nuclear medicine, radio-therapeutics for RIT (RadioIsotope Therapy) and radio-tracers for molecular imaging experiments such as PET (Positron Emission Tomography), SPECT (Single Photon Emission Computed Tomography) or scintigraphy have been described. Several useful isotopes of iodine can be used for both diagnosis and therapy: 123 I for SPECT imaging, 124 I for PET imaging, 125 I for biological assays and 131 I for radio-therapy and scintigraphy. Classical methods of radioiodination methods use a prefunctionalized precursor, which must be synthesized, isolated and purified before being introduced to the radio-iodination step. The radioiododestannylation method is the most popular method, although stannylated precursors are known for their difficult synthesis and their toxicity. The development of new methods of radioiodination is therefore of great interest in the field of radiochemistry. Based on a previous work, our group has developed a method to radio-iodinate N-acylsulfonamides through a room temperature palladium mediated C-H radio-iodination. This original strategy allows radiolabeling of biomolecules in very mild conditions without the use of chemical precursors. Based on literature, our group is now developping a new method to radio-iodinate arylsilyl derivates through radioiododesilylation in mild conditions, Radio-iodation, radioligand, activation C-H, radioiodésilylation Development of new radioiodination techniques and application to the radiolabeling of molecules of interest Labeling of (bio)molecules with radioactive isotopes is of high interest to for the scientific community, as it strongly impacts the discovery process in life science and nuclear medicine